Syntheses and Biological Activities of Polymers Containing 3′-Azido-3′-deoxythymidine

✍ Scribed by Choi, Won-Moon; Lee, Neung-Ju; Ha, Chang-Sik; Cho, Won-Jei

• Publisher: John Wiley and Sons
• Year: 1997
• Tongue: English
• Weight: 361 KB
• Volume: 43
• Category: Article
• ISSN: 0959-8103
• DOI: 10.1002/(sici)1097-0126(199706)43:2<167::aid-pi733>3.0.co;2-m

✦ Synopsis

The new monomer, 5@-O-methacryloyl-3@-azido-3@-deoxythymidine (MAZT), was synthesized by the reaction of methacryloyl chloride and 3@-azido-3@-deoxythymidine (AZT). Poly(MAZT) and copolymers of MAZT with vinyl acetate (VAc) and maleic anhydride (MAH) were synthesized by radical polymerizations. The synthesized MAZT and polymers were identiÐed by 1H nuclear magnetic resonance (NMR), 13C NMR, elemental analysis and gel permeation chromatography. The quantities of MAZT units in poly(MAZT-co-VAc) and poly(MAZT-co-MAH) were 45 and 27 mol%, respectively. The weight average molecular weights of the polymers synthesized were in the range from 8800 to 17 600. The in vitro cytotoxicities of samples against K562 human leukaemia cell line at 100 kg ml~1 decreased in the following order : poly(MAZT-co-MAH) [ poly(MAZT-co-VAc) [ poly(MAZT) [ MAZT [ AZT. The in vivo antitumour activities of the polymers synthesized against Balb/C mice bearing sarcoma 180 tumour cells were greater than those of 5-Ñuorouracil at all concentrations.